OXTRIPHYLLINE PEDIATRIC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OXTRIPHYLLINE PEDIATRIC (OXTRIPHYLLINE PEDIATRIC).
Xanthine derivative that inhibits phosphodiesterase, increasing cyclic AMP levels; antagonizes adenosine receptors, leading to bronchodilation, central nervous system stimulation, and positive inotropic effects.
| Metabolism | Hepatic via CYP1A2, CYP2E1, and CYP3A4; major metabolite is 1-methyl-3-propylxanthine; exhibits non-linear kinetics at high doses. |
| Excretion | Renal (70-80% as unchanged drug, 10-15% as metabolites); biliary/fecal (<10%) |
| Half-life | Neonates: 24-36 hours; Infants 1-6 months: 14-29 hours; Children 6-12 months: 9-18 hours; Children 1-9 years: 3-6 hours; Adults: 7-12 hours. Half-life prolonged in hepatic impairment, CHF, and COPD. |
| Protein binding | 55-65% (primarily albumin). |
| Volume of Distribution | 0.4-0.6 L/kg (increased in premature neonates and hepatic disease). |
| Bioavailability | Oral immediate-release: 90-100%; Sustained-release: 80-95% (relative to immediate-release). |
| Onset of Action | Oral (immediate-release): 30-60 minutes on empty stomach; 60-90 minutes with food. Intravenous: 15-30 minutes. |
| Duration of Action | Oral (immediate-release): 4-6 hours; Sustained-release: 8-12 hours. Variable with formulation and individual metabolism. |
200 mg orally every 6-8 hours; extended-release: 400-600 mg orally every 12 hours.
| Dosage form | SYRUP |
| Renal impairment | No specific guidelines; consider dose reduction in severe renal impairment (GFR <30 mL/min) to avoid accumulation. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: reduce dose by 75% or avoid use. |
| Pediatric use | 1-9 years: 4 mg/kg/dose orally every 6 hours; 9-16 years: 3 mg/kg/dose orally every 6 hours; adjust based on serum theophylline levels (target 5-15 mcg/mL). |
| Geriatric use | Start at 200 mg orally every 12 hours (extended-release) and titrate slowly; monitor serum theophylline levels closely due to reduced clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OXTRIPHYLLINE PEDIATRIC (OXTRIPHYLLINE PEDIATRIC).
| Breastfeeding | Theophylline (active metabolite) is excreted into breast milk; M/P ratio approximately 0.6-0.8. Peak milk concentration occurs 2-3 hours after dose. Recommendations: Caution in preterm infants due to immature clearance; observe for irritability, insomnia, or feeding intolerance. Avoid if maternal dose exceeds moderate levels. |
| Teratogenic Risk | Oxtriphylline, a theophylline derivative, is classified as pregnancy category C. First trimester: Limited data, no known major malformations in humans; animal studies show no teratogenicity at clinically relevant doses. Second and third trimesters: No specific risks, but maternal respiratory depression and fetal tachycardia may occur with high doses. Perinatal: Apnea, irritability, and jitteriness reported in neonates due to transplacental passage. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Hypersensitivity to oxitriphylline or any xanthine","Active peptic ulcer disease","Seizure disorder (unless adequately controlled)"]
| Precautions | ["Risk of toxicity (seizures, cardiac arrhythmias) at serum levels >20 mcg/mL","Reduce dose in hepatic impairment, heart failure, and with drugs that inhibit metabolism (e.g., cimetidine, ciprofloxacin)","Monitor serum theophylline concentrations"] |
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| Fetal Monitoring | Maternal: Serum theophylline levels (target 5-15 mcg/mL), heart rate, respiratory rate, signs of toxicity (tachycardia, nausea, seizures). Fetal/neonatal: Heart rate monitoring for tachycardia (maternal high levels), assessment for apnea or irritability in newborns if exposed near term. |
| Fertility Effects | No evidence of impaired fertility in humans. Animal studies: No adverse effects on reproductive function at therapeutic doses. |